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1. Ampicillin concentrations in cyst wall (wall) and cyst fluid (fluid) of radicular cyst and serum following a single oral administration of bacampicillin (equivalent to 500 mg of ampicillin) were measured by a paper disk method. 2. The mean peak concentrations of ampicillin in wall, fluid, and serum occurred at identical times, 1.5 hr, and were 2.39 micrograms/g, 0.77, and 10.24 micrograms/ml, respectively. 3. Mean ampicillin concentration ratios of wall/serum, fluid/serum, and fluid/wall at the peak time were 0.23, 0.07, and 0.40, respectively. 4. Mean ampicillin concentrations in wall and fluid at the peak time exceeded MIC (minimum inhibitory concentration) for 90% (0.5 microgram/ml) for clinically isolated strains of alpha-hemolytic Streptococci.

The concentrations of ampicillin in serum and mixed saliva after a single oral administration of lenampicillin (500 mg) were determined by the paper disc method. The samples of serum and mixed saliva were obtained at 1, 2, 3 and 4 h after administration. The highest concentrations of ampicillin in serum and mixed saliva occurred 1 h after administration of lenampicillin, and were 11.55 and 0.060 micrograms/ml, respectively. A significant correlation coefficient between the concentrations of ampicillin in serum and mixed saliva, r = 0.71, P less than 0.001, was found.

The concentrations of ampicillin (ABPC) from talampicillin (TAPC) and cefadroxil (CDX) in serum and mixed saliva were assayed by the thin layer disc plate method. Talampicillin and cefadroxil (500 mg) were given by a single oral administration. The relationships between serum and mixed saliva ampicillin and cefadroxil concentrations were evaluated in the paired specimens collected from 10 different persons, respectively. The means of concentration ratios of mixed saliva to serum ampicillin and cefadroxil were 0.006 +/- 0.003 and 0.025 +/- 0.010 (mean +/- SD), respectively. Significant correlation coefficients between mixed saliva and serum concentrations were found for both ampicillin and cefadroxil, which were r = 0.78, P less than 0.001, and r = 0.67, P less than 0.001, respectively.

Ampicillin concentrations in human serum and periodontal membrane after a single oral administration of bacampicillin (500 mg) were assayed by the agar diffusion (paper disc) method. The peak times of serum and periodontal membrane were nearly identical, being approx. 90 min after administration. The peak concentrations of serum and periodontal membrane were 12.81 micrograms/ml and 6.97 micrograms/g, respectively. The concentration ratio of periodontal membrane to serum at the peak time was 0.56.

Ninety-six patients who underwent the extraction of impacted mandibular third molars in a nonfasting state were given a single oral dose of bacampicillin preoperatively. Specimens of serum from venous blood (n = 107), gingiva (n = 57), mandibular bone (n = 68), dental follicle (n = 56), and dental pulp (n = 43) were obtained during the operation and assayed for ampicillin content. The mean peak concentrations in serum, gingiva, mandibular bone, dental follicle, and dental pulp all occurred approximately 90 minutes after administration. The concentration ratios of the tissues to the corresponding serum at the peak time were 0.50, 0.20, 0.34, and 0.61, respectively. Bacampicillin showed good absorption by the intestine, and sufficient concentrations of the resulting metabolite, ampicillin, were found in the oral tissues.

1. Ampicillin concentrations in human serum and periodontal membrane after a single oral administration of talampicillin (500 mg) were assayed by the agar diffusion (paper disc) method. 2. The peak times of serum and periodontal membrane were identical, being 150 min after administration. 3. The peak concentrations of serum and periodontal membrane were 7.81 micrograms/ml and 4.11 micrograms/g, respectively. 4. The mean ratio of periodontal membrane to serum concentration at the peak time was 0.53.

Ampicillin concentrations in human serum and dental granulomas of 31 patients were determined after a single oral dose of talampicillin (equivalent to 500 mg of ampicillin) was administered to each. The specimens were taken at 1.5, 2.0, 2.5, 3.0, and 3.5 h after the administration of talampicillin. The mean peak ampicillin concentrations in serum and dental granulomas occurred at identical times, 2.5 h, and were 8.29 micrograms/ml (range, 1.81 to 13.20 micrograms/ml) and 2.94 micrograms/g (range, 1.14 to 7.16 micrograms/g), respectively. The mean dental granuloma/serum ampicillin concentration ratio at the peak time (2.5 h) was 0.42 (range, 0.29 to 0.56). Ampicillin concentrations in dental granulomas exceeded most of the MICs for the bacteria commonly isolated from odontogenic infection.

Ampicillin (ABPC) concentrations in human serum, gingiva, the mandibular bone, and dental follicle after a single oral administration of ampicillin (500 mg) were assayed by the agar diffusion (paper disc) method. The peak times of all specimens were identical, being 120 min after administration. The peak concentrations of the respective specimens were 2.01 micrograms/ml, 1.03, 0.34, and 0.72 micrograms/g, respectively. The concentration ratios of gingiva, the mandibular bone, and dental follicle to their corresponding serum at the peak time were 0.51, 0.16, and 0.35, respectively.

The antibacterial activities, absorption and excretion of talampicillin hydrochloride were compared with those of amoxicillin and ampicillin. Talampicillin hydrochloride showed a broad-spectrum antibacterial activity against Gram-positive and Gram-negative bacteria as seen in amoxicillin and ampicillin. The antibacterial activities of talampicillin hydrochloride, amoxicillin and ampicillin were quite similar. In experimental murine infection with Staphylococcus aureus, protective effect of talampicillin hydrochloride was superior to ampicillin. For Escherichia coli infection, protective effect of talampicillin hydrochloride was similar to that of amoxicillin, while ampicillin was less active than both talampicillin hydrochloride and amoxicillin. The absorption and excretion of 250 mg equivalent doses of talampicillin hydrochloride, amoxicillin and ampicillin were compared in nine fasting healthy volunteers after oral administration of these antibiotics in randomized triple crossover study. In order to calculate the pharmacokinetic parameters, plasma levels were analyzed using an one-compartment open model, as well as area under the plasma concentration curve (AUC) and urinary excretion. Maximum plasma levels calculated were 2.8 times higher for talampicillin hydrochloride and 1.45 times higher for amoxicillin than for ampicillin. AUC was greater for talampicillin hydrochloride than for amoxicillin and lowest for ampicillin. Urinary excretion of talampicillin hydrochloride as penicillin determined in biological assay was comparable to that of amoxicillin and 1.55 times higher than that of ampicillin. Penicillins can be metabolized to penicilloic acids in the body. After taking into account the penicilloic acid contents in urine, total excretion in urine was 61% for talampicillin hydrochloride, 67% for amoxicillin and 42% for ampicillin during 6 hours after dosing. The absorption of the drugs was evaluated according to the plasma levels, the area under plasma concentration curve and the percentage of excretion in urine. The results obtained showed that talampicillin hydrochloride was well absorbed from the gastro-intestinal tract.